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公开(公告)号：US08669277B2
公开(公告)日：2014-03-11
申请号：US13265138
申请日：2010-04-19
IPC分类号： A61K31/454 , C07D417/14
CPC分类号： C07D417/14 , A01N43/653 , A01N43/80 , A01N43/84 , A01N57/12 , A01N59/20
摘要： Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed.Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed.Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.
摘要翻译： 公开了1- [4- [4- [5-（2,6-二氟苯基）-4,5-二氢-3-异恶唑基] -2-噻唑基] -1-哌啶基] -2- [5- （三氟甲基）-1H-吡唑-1-基]乙酮（化合物1）。 公开了制备化合物1的固体形式和将一种固体形式的化合物1转化成另一种的方法。 公开了包含杀真菌有效量的固体形式的化合物1和至少一种选自表面活性剂，固体稀释剂和液体载体的另外的组分的杀真菌组合物。 还公开了包含固体形式的化合物1和至少一种其它杀真菌剂或杀虫剂的混合物的组合物。 还公开了用于控制由真菌植物病原体引起的植物疾病的方法，包括向植物或其部分或植物种子施用杀真菌有效量的化合物1的固体形式。
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公开(公告)号：US20120034315A1
公开(公告)日：2012-02-09
申请号：US13265138
申请日：2010-04-19
IPC分类号： A01N59/20 , A61K31/454 , A01N43/90 , A01N43/54 , A01P7/04 , A01N57/12 , A01N57/10 , A01N43/42 , A01P3/00 , C07D417/14 , A01N55/10
CPC分类号： C07D417/14 , A01N43/653 , A01N43/80 , A01N43/84 , A01N57/12 , A01N59/20
摘要： Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed.Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed.Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.
摘要翻译： 公开了1- [4- [4- [5-（2,6-二氟苯基）-4,5-二氢-3-异恶唑基] -2-噻唑基] -1-哌啶基] -2- [5- （三氟甲基）-1H-吡唑-1-基]乙酮（化合物1）。 公开了制备化合物1的固体形式和将一种固体形式的化合物1转化成另一种的方法。 公开了包含杀真菌有效量的固体形式的化合物1和至少一种选自表面活性剂，固体稀释剂和液体载体的另外的组分的杀真菌组合物。 还公开了包含固体形式的化合物1和至少一种其它杀真菌剂或杀虫剂的混合物的组合物。 还公开了用于控制由真菌植物病原体引起的植物疾病的方法，包括向植物或其部分或植物种子施用杀真菌有效量的化合物1的固体形式。
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公开(公告)号：US08871939B2
公开(公告)日：2014-10-28
申请号：US13981919
申请日：2012-01-27
IPC分类号： C07C231/10 , C07D231/14 , C07D401/04
CPC分类号： C07C231/02 , C07C231/10 , C07D231/14 , C07D401/04 , C07C237/30
摘要： A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure. A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.
摘要翻译： 制备式1化合物的方法，包括在钯源，配体，碱和一氧化碳的存在下使式2和3的化合物接触，其中R 1，R 2，X和R 3如本公开所定义。 制备式5化合物的方法，其中R 1，R 2，R 3，R 4，R 5，R 6和Z如本公开所定义，使用式1化合物，其特征在于通过上述方法制备式1化合物或式 使用通过上述方法制备的式1的化合物。
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公开(公告)号：US20130310567A1
公开(公告)日：2013-11-21
申请号：US13981919
申请日：2012-01-27
IPC分类号： C07C231/10 , C07D231/14 , C07D401/04
CPC分类号： C07C231/02 , C07C231/10 , C07D231/14 , C07D401/04 , C07C237/30
摘要： A method for preparing a compound of Formula 1 comprising contacting a compound of Formulae 2 and 3 in the presence of a palladium source, a ligand, a base and carbon monoxide wherein R1, R2, X and R3 are as defined in the disclosure.A method for preparing a compound of Formula 5 wherein R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 characterized by preparing a compound of Formula 1 by the method disclosed above or using a compound of Formula 1 prepared by the method above.
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公开(公告)号：US20110184183A1
公开(公告)日：2011-07-28
申请号：US13121218
申请日：2009-11-11
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： A method is disclosed for preparing a non-hydratable crystal form from a hydratable crystal form of 3-bromo-1-(3-chloro-2-pyridinyl)-N-[4-cyano-2-methyl-6-[(methylamino)-carbonyl]phenyl]-1H-pyrazole-5-carboxamide (Compound 1).
摘要翻译： 公开了从可水合的3-溴-1-（3-氯-2-吡啶基）-N- [4-氰基-2-甲基-6 - [（甲基氨基） ） - 羰基]苯基] -1H-吡唑-5-甲酰胺（化合物1）。
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公开(公告)号：US08410278B2
公开(公告)日：2013-04-02
申请号：US13121218
申请日：2009-11-11
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： A method is disclosed for preparing a non-hydratable crystal form from a hydratable crystal form of 3-bromo-1-(3-chloro-2-pyridinyl)-N-[4-cyano-2-methyl-6-[(methylamino)-carbonyl]phenyl]-1H-pyrazole-5-carboxamide (Compound 1).
摘要翻译： 公开了从可水合的3-溴-1-（3-氯-2-吡啶基）-N- [4-氰基-2-甲基-6 - [（甲基氨基） ） - 羰基]苯基] -1H-吡唑-5-甲酰胺（化合物1）。
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公开(公告)号：US07402296B2
公开(公告)日：2008-07-22
申请号：US11661516
申请日：2005-08-30
CPC分类号： C01G3/02 , A01N59/20 , C01P2006/60 , C01P2006/64 , A01N59/26 , A01N25/22 , A01N2300/00
摘要： Disclosed is a method of stabilizing copper(II) hydroxide, the method comprising the sequential steps of: (a) combining copper(II) hydroxide, a water-soluble phosphate and water to form a mixture; and (b) drying the mixture. Also disclosed is stabilized copper(II) hydroxide prepared according to said method and a composition comprising stabilized copper(II) hydroxide prepared according to said method and at least one of a surfactant, a solid diluent or a liquid diluent.
摘要翻译： 公开了一种稳定氢氧化铜（II）的方法，该方法包括以下顺序步骤：（a）将氢氧化铜（II），水溶性磷酸盐和水混合以形成混合物; 和（b）干燥混合物。 还公开了根据所述方法制备的稳定化的氢氧化铜（II），以及包含根据所述方法制备的稳定的氢氧化铜（II）和表面活性剂，固体稀释剂或液体稀释剂中的至少一种的组合物。
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